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Showing 1–7 of 7 results
Advanced filters: Author: Jet Tsien Clear advanced filters

  • The pentafluorosulfanyl group has been long considered a potential (bio)isostere for tert-butyl and trifluoromethyl groups, yet limitations in methodologies have constrained access to it. Here, the authors report a general pentafluorosulfanylation platform that employs bench-stable solid reagents to generate SF5 radicals via a decarboxylation and β-scission sequence.

    • Renzhe Li
    • Chang Liu
    • Tian Qin
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-8

  • The bicyclo[1.1.1]pentane (BCP) motif has drawn increasing attention recently in drug discovery. Now, a programmable bis-functionalization strategy has been developed to modularly access bridge-substituted BCP scaffolds, based on the inherent chemoselectivity of BCP bis-boronates (3° > 2°). This strategy should enable further structure–activity relationship studies of BCP-containing drug candidates and open the door to unexplored chemical space.

    • Yangyang Yang
    • Jet Tsien
    • Tian Qin
    Research
    Nature Chemistry
    Volume: 16, P: 285-293

  • Direct and stereospecific C(sp3)–C(sp2) cross-coupling reactions are highly desirable for the construction of complex molecular scaffolds. Now, using stable and easily accessible alkyl sulfinates as coupling reagents, a modular and programmable sulfurane-mediated coupling method has been developed for the installation of various hindered alkyl bioisosteres, such as trifluoromethyl cyclopropyl, to (hetero)aromatics.

    • Min Zhou
    • Jet Tsien
    • Tian Qin
    Research
    Nature Chemistry
    Volume: 15, P: 550-559

  • Readily accessible enantioenriched sulfonylhydrazides and low loadings of an inexpensive achiral Ni catalyst can be used to control the stereochemical outcome of radical cross-coupling.

    • Jiawei Sun
    • Jiayan He
    • Phil S. Baran
    Research
    Nature
    Volume: 642, P: 85-91

  • Bicyclic hydrocarbons, and bicyclo[1.1.1]pentanes in particular, are playing an emerging role as saturated bioisosteres in pharmaceutical, agrochemical and materials intramolecular coupling approach has been developed for the modular construction of underexplored multisubstituted strained bicyclic hydrocarbons, ranging from [1.1.1] to [3.2.1] scaffolds.

    • Yangyang Yang
    • Jet Tsien
    • Tian Qin
    Research
    Nature Chemistry
    Volume: 13, P: 950-955

  • In this Review, synthetic approaches to polycyclic scaffolds, which can act as saturated, three-dimensional bioisosteric replacements of ortho-substituted, meta-substituted and multi-substituted benzenes, are discussed. Their application in medicinal chemistry is also summarized.

    • Jet Tsien
    • Chao Hu
    • Tian Qin
    Reviews
    Nature Reviews Chemistry
    Volume: 8, P: 605-627